There is considerable interest in the pharmacological effects and metabolism of apomorphine alkaloids in general, and apomorphine in particular. Apomorphine has been shown to be therapeutically beneficial in the treatment of Parkinson's disease and schizophrenia. However, apomorphine possesses a short half-life in patients, is effectively active only when administered parenterally, and reportedly causes azotemia in a significant number of patients during chronic therapy. Recent studes in our laboratory suggest that the rabbit may serve as a good animal model for apomorphine-induced azotemia. We have also found that apomorphine's poor oral activity in rodents (and perhaps in man) is due to very rapid metabolism in the liver (a so-called "first-pass effect"). This work has been aided by specifically radiolabelled apomorphine prepared in our laboratories and by pharmacological tests that monitor dopaminergic activity of apomorphine in mice. Analytical methods are being developed that should help describe the disposition of apomorphine in animals and in man. These procedures will also aid in the development of apomorphine prodrugs which may ultimately be useful in human medicine.